Abstract
We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Alzheimer Disease / drug therapy*
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Amyloid Precursor Protein Secretases / antagonists & inhibitors*
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Amyloid Precursor Protein Secretases / chemistry
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Drug Design
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Humans
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Molecular Structure
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry*
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Protein Conformation
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfones / chemical synthesis
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Sulfones / chemistry*
Substances
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Protease Inhibitors
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Sulfonamides
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Sulfones
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Amyloid Precursor Protein Secretases